| Identification | Back Directory | [Name]
4SC-202 | [CAS]
1186222-89-8 | [Synonyms]
4SC-202
CS-1272
4SC-202 tosylate
Domatinostat tosylate
4SC-202;4SC202;4SC 202
(E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide 4-methylbenzenesulfonate
4SC-202 2-Propenamide, N-(2-aminophenyl)-3-[1-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]sulfonyl]-1H-pyrrol-3-yl]-, (2E)-, 4-methylbenzenesul | [Molecular Formula]
C30H29N5O6S2 | [MDL Number]
MFCD25976779 | [MOL File]
1186222-89-8.mol | [Molecular Weight]
619.711 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥2.4 mg/mL in EtOH with gentle warming and ultrasonic; ≥62 mg/mL in DMSO | [form ]
Powder | [color ]
Light yellow to brown |
| Hazard Information | Back Directory | [Description]
4SC-202 is an inhibitor of the class I histone deacetylases (HDACs) HDAC1-3 and the histone demethylase KDM1A. It reduces cell viability in a panel of colorectal cancer (CRC) cell lines when used at concentrations ranging from 1 to 10 μM and in patient-derived CRC cell lines when used at a concentration of 5 μM. 4SC-202 (5 μM) induces cell cycle arrest at the G2/M phase in HT-29 cells and primary human CRC cells and increases apoptosis in HT-29 cells in a concentration-dependent manner, an effect that is enhanced by the Akt inhibitors perifosine and MK-2206 . 4SC-202 (100 mg/kg, p.o., every other day) reduces tumor growth in an HT-29 mouse xenograft model when administered alone and to an enhanced degree when co-administered with oxaliplatin (Item No. 13106). | [in vivo]
studies, 4sc-202 has shown a good tolerability and dose-dependent effect on anti-tumour activity compared with other inhibitors in the a549nsclc xenograft model and the rko27 colon carcinoma model [1]. | [References]
[1] henning s w, doblhofer r, kohlhof h, et al. 178 preclinical characterization of 4sc-202, a novel isotype specific hdac inhibitor[j]. european journal of cancer supplements, 2010, 8(7): 61. |
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